Abstract
Histone deacetylases (HDACs) are key enzymes in the regulation of gene expression. By maintaining the dynamic equilibrium of the acetylation status of highly conserved lysine residues on histones, they regulate chromatin remodeling and gene expression. A link between aberrant HDAC activity and cancer has been widely reported and HDAC inhibitors have been shown to inhibit the proliferation of human tumor cell lines in vitro. Furthermore, several HDAC inhibitors have exhibited potent anti-tumor activity in human xenograft models, suggesting this class of compounds to be promising novel cancer therapeutic agents. This review provides an update on the current knowledge of HDAC inhibition with a focus on the most recent progress of HDAC inhibitors in clinical development.
Keywords: chromatin, histone acetylation, anti-cancer
Current Medicinal Chemistry
Title: Histone Deacetylase Inhibitors: From Chromatin Remodeling to Experimental Cancer Therapeutics
Volume: 10 Issue: 22
Author(s): Janine Arts, Stefanie de Schepper and Kristof Van Emelen
Affiliation:
Keywords: chromatin, histone acetylation, anti-cancer
Abstract: Histone deacetylases (HDACs) are key enzymes in the regulation of gene expression. By maintaining the dynamic equilibrium of the acetylation status of highly conserved lysine residues on histones, they regulate chromatin remodeling and gene expression. A link between aberrant HDAC activity and cancer has been widely reported and HDAC inhibitors have been shown to inhibit the proliferation of human tumor cell lines in vitro. Furthermore, several HDAC inhibitors have exhibited potent anti-tumor activity in human xenograft models, suggesting this class of compounds to be promising novel cancer therapeutic agents. This review provides an update on the current knowledge of HDAC inhibition with a focus on the most recent progress of HDAC inhibitors in clinical development.
Export Options
About this article
Cite this article as:
Arts Janine, Schepper de Stefanie and Emelen Van Kristof, Histone Deacetylase Inhibitors: From Chromatin Remodeling to Experimental Cancer Therapeutics, Current Medicinal Chemistry 2003; 10 (22) . https://dx.doi.org/10.2174/0929867033456657
DOI https://dx.doi.org/10.2174/0929867033456657 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
Call for Papers in Thematic Issues
Advances in Medicinal Chemistry: From Cancer to Chronic Diseases.
The broad spectrum of the issue will provide a comprehensive overview of emerging trends, novel therapeutic interventions, and translational insights that impact modern medicine. The primary focus will be diseases of global concern, including cancer, chronic pain, metabolic disorders, and autoimmune conditions, providing a broad overview of the advancements in ...read more
Approaches to the treatment of chronic inflammation
Chronic inflammation is a hallmark of numerous diseases, significantly impacting global health. Although chronic inflammation is a hot topic, not much has been written about approaches to its treatment. This thematic issue aims to showcase the latest advancements in chronic inflammation treatment and foster discussion on future directions in this ...read more
Cellular and Molecular Mechanisms of Non-Infectious Inflammatory Diseases: Focus on Clinical Implications
The Special Issue covers the results of the studies on cellular and molecular mechanisms of non-infectious inflammatory diseases, in particular, autoimmune rheumatic diseases, atherosclerotic cardiovascular disease and other age-related disorders such as type II diabetes, cancer, neurodegenerative disorders, etc. Review and research articles as well as methodology papers that summarize ...read more
Chalcogen-modified nucleic acid analogues
Chalcogen-modified nucleosides, nucleotides and oligonucleotides have been of great interest to scientific research for many years. The replacement of oxygen in the nucleobase, sugar or phosphate backbone by chalcogen atoms (sulfur, selenium, tellurium) gives these biomolecules unique properties resulting from their altered physical and chemical properties. The continuing interest in ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Marginal Vitamin A Deficiency Exacerbates Memory Deficits Following Aβ1-42 Injection in Rats
Current Alzheimer Research Small-molecule Modulation of HDAC6 Activity: The Propitious Therapeutic Strategy to Vanquish Neurodegenerative Disorders
Current Medicinal Chemistry Novel Concepts in the Pathogenesis and Management of Pediatric Hypertension
Current Pediatric Reviews Dietary Phytochemicals in Chemoprevention of Cancer: An Update
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) Gas1 is a Pleiotropic Regulator of Cellular Functions: from Embryonic Development to Molecular Actions in Cancer Gene Therapy
Mini-Reviews in Medicinal Chemistry Intracellular Accumulation of Toxic Turn Amyloid-β is Associated with Endoplasmic Reticulum Stress in Alzheimer’s Disease
Current Alzheimer Research The Therapeutic Potential of Purinergic Receptors in Alzheimer’s Disease and Promising Therapeutic Modulators
Mini-Reviews in Medicinal Chemistry Signaling Epicenters: The Role of Caveolae and Caveolins in Volatile Anesthetic Induced Cardiac Protection
Current Pharmaceutical Design Interleukin-15 in Gene Therapy of Cancer
Current Gene Therapy The Role of Cnidaria in Drug Discovery. A Review on CNS Implications and New Perspectives
Recent Patents on CNS Drug Discovery (Discontinued) The Effect of PAOPA, a Novel Allosteric Modulator of Dopamine D2 Receptors, on Signaling Proteins Following Sub-Chronic Administration in Rats
Current Molecular Pharmacology Neuronal and Vascular Oxidative Stress in Alzheimers Disease
Current Neuropharmacology Protective Effects of Chronic Green Tea Consumption on Age-related Neurodegeneration
Current Pharmaceutical Design Beyond Estrogen: Targeting Gonadotropin Hormones in the Treatment of Alzheimers Disease
Current Drug Targets - CNS & Neurological Disorders Inhibition of Key Fungal (02) Protein(s) (Aspergillus fumigatus) In-Response to Treatment with Poly-Acid Ligand
Current Proteomics Immunotherapy of Cancer Based on DC-Tumor Fusion Vaccine
Current Immunology Reviews (Discontinued) Imaging of EGFR and EGFR Tyrosine Kinase Overexpression in Tumors by Nuclear Medicine Modalities
Current Pharmaceutical Design Cyclophilin A as a Target of Cisplatin Chemosensitizers
Current Cancer Drug Targets Regulation of Transcription Factors by Heterotrimeric G Proteins
Current Molecular Pharmacology Proline-Rich Peptides: Multifunctional Bioactive Molecules as New Potential Therapeutic Drugs
Current Protein & Peptide Science